“angiotensin receptors”的搜索结果
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LXR-like receptors 激动剂
GW3965 HCl是一种选择性的口服活性肝X受体(LXR)完全激动剂。
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- Mohácsik P, .et al. A Transgenic Mouse Model for Detection of Tissue-Specific Thyroid Hormone Action, Endocrinology, 2018, Feb 1;159(2):1159-1171 PMID: 29253128
- Pencheva N, .et al. Broad-spectrum therapeutic suppression of metastatic melanoma through nuclear hormone receptor activation., Cell., 2014, 156(5):986-1001 PMID: 24581497
- Bin Dong, .et al. High-fructose diet downregulates long-chain acyl-CoA synthetase 3 expression in liver of hamsters via impairing LXR/RXR signaling pathway, J Lipid Res., 2013, May; 54(5): 1241-1254. PMID: 23427282
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Opioid Receptors 激动剂
BRL 52537 hydrochloride是一种高度选择性和有效的κ阿片类激动剂(Ki = 0.24 nM)。比吗啡强25倍。
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5-HT Receptors 拮抗剂
Ondansetron HCl (GR 38032F)是5-羟色胺5-HT3受体拮抗剂,主要用作止吐药,通常在化疗后用于治疗恶心和呕吐。
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5-HT Receptors/D2 dopamine receptor 拮抗剂
Olanzapine (LY170053)对5-HT2血清素和D2多巴胺受体拮抗剂具有高亲和力。
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mGlu4 receptors modulator
VU 0361737是mGluR-4的选择性正变构调节剂(人和大鼠受体的EC50值分别为240和110 nM)。
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GABAB receptors 拮抗剂
2-Hydroxysaclofen对GABAB受体是一种有效的选择性拮抗剂。
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adenosine A2B receptors 拮抗剂
CVT-6883是一种选择性的A2B腺苷拮抗剂,代表了一种治疗心肺疾病的新型潜在方法。
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NMDA receptors 拮抗剂
NVP-AAM077抑制成年小鼠在脑室下区域和齿状回中的祖细胞增殖,并降低了齿状回中的新生细胞的存活。
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alpha1/beta adrenergic receptors 拮抗剂
Labetalol HCl是选择性α1-肾上腺素能受体和非选择性β-肾上腺素能受体的双重拮抗剂。
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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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β3-adrenergic receptors 激动剂
BRL 37344 Na Salt是具有脂解活性的β3-AR(β3-肾上腺素能受体)选择性激动剂。
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β-adrenergic receptors 激动剂
Cimaterol是β的有效激动剂;肾上腺素能受体(人β的pEC50 = 8.13、8.78和6.62;1β,2β和3β)。
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TGF-β Receptors 抑制剂
SB-505124 Hydrochloride是激活素受体样激酶(ALKS)的抑制剂。
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NMDA receptors Potentiator
CIQ是包含NR2C或NR2D亚基的NMDA受体的亚基选择性增强剂。
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M3 receptors 抑制剂
Imidafenacin是一种有效的选择性M3受体抑制剂,Kb为0.317 nM。对M2受体的效力较低(IC50 = 4.13 nM)。
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NMDA receptors blocker
RO 25-6981 maleate是含有NR2B亚基的NMDA受体的强效和选择性活性依赖性阻断剂。克隆的受体亚基组合NR1C/NR2B和NR1C/NR2A的IC50值分别为0.009和52 uM。
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mGlu4 receptors modulator
VU 0364770是mGlu4受体的正变构调节剂,在表达mGlu4的HEK 293细胞中EC50值为290 nM。
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β-adrenergic receptors 拮抗剂
Acebutolol HCl是一种β-肾上腺素能受体拮抗剂,用于治疗高血压,心绞痛和心律不齐。
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NMDA receptors Blocker
Ro 25-6981是N-甲基-D-天冬氨酸(NMDA)受体的高亲和力,强效选择性阻断剂。
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A1 adenosine receptors 拮抗剂
Proxyphylline是茶碱的衍生物,由于其心血管特性而被用作支气管扩张剂。它与A2腺苷受体(对于血小板,Ki = 850μM)选择性拮抗A1腺苷受体(对于牛脑,Ki = 82 nM)。
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CCR2/5 receptors 抑制剂
Cenicriviroc(TAK-652,TBR-652)是CCR2和CCR5受体的抑制剂,可使其充当防止病毒进入人细胞的进入抑制剂
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H3 receptors
S38093 HCl是组胺H3受体的反向激动剂。
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GABA receptor agonist
Afloqualone, also known as HQ-495, is a centrally acting muscle relaxant. Afloqualone inhibits vestibular nystagmus probably due to both inhibition of selective polysynaptic transmission and enhancement of the effects of GABA and glycine in the lateral vestibular nucleus (LVN), and its GABA-enhancing effect is thought to be attributable to the increased sensitivity of GABA receptors of the LVN neuron site.
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Dopamine receptor antagonist
Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
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Picrotoxinin negatively modulate the action of GABA on GABAA receptors.
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α-1 adrenergic receptor blocker
Doxazosin is an α-1 adrenergic receptor blocker that inhibits the binding of norepinephrine, which is released from sympathetic nerve terminals, to the α-1 receptors on the membrane of vascular smooth muscle cells. Blockages of the alpha-1 adrenergic action on the vascular smooth muscles lead to a decrease in vascular resistance and antihypertensive activity.
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Sertindole is one of the newer antipsychotic medications and a neuroleptic. Like the other atypical antipsychotics, it has activity at dopamine and serotonin receptors in the brain. It is used in the treatment of schizophrenia.
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Bradykinin B2 receptors antagonist
Icatibant (HOE-140) is a selective and specific antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively.
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mAChR agonist
Cevimeline (Evoxac) Hcl is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors; used in the treatment of dry mouth associated with sjogren's syndrome.
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Tetracaine is a potent local anesthetic. It alters the function of calcium release channels (ryanodine receptors) that control the release of calcium from intracellular stores.
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5-HT receptor antagonist
Pizotifen is a serotonin antagonist which acts mainly at the 5-HT1, 5-HT2A, and 5HT2C receptors with some antihistamine activity.
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Peretinoin, also known as NIK-333 , orally available, acyclic retinoid with potential antineoplastic and chemopreventive activities. Peretinoin binds to and activates nuclear retinoic acid receptors (RAR), which in turn recruit coactivator proteins and promote, with other transcriptional complexes, the transcription of target genes. As a result, this agent may modulate the expression of genes involved in the regulation of cell proliferation, cell differentiation, and apoptosis of both normal and tumor cells.
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GABA agonist
Baclofen is a GABA agonist specific for GABA-B receptors. Baclofen is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing It acts at spinal and supraspinal sites, reducing excitatory transmission.
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Flurandrenolide is a synthetic glucocorticoid with anti-inflammatory and anti-allergic properties. Flurandrenolide exerts its effects by interacting with specific cytoplasmic glucocorticoid receptors and subsequently activates glucocorticoid receptor mediated gene expression.
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Metergoline is a psychoactive drug of the ergoline chemical class which acts as a ligand for various serotonin and dopamine receptors.
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neuropeptide Y1 receptor antagonist
BMS-193885 is a potent, competitive neuropeptide (NPY) Y1 antagonist (Ki = 3.3 nM, IC50 = 5.9 nM) that displays > 47, > 100, > 160, > 160 and > 160-fold selectivity over ??1, α1, Y2, Y4 and Y5 receptors respectively.
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Glucocorticoid Receptor Antagonist
OP-3633 is a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (IC50 = 29 nM).
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Muscarinic agonist
Cevimeline (AF-102B) is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors; used in the treatment of dry mouth associated with sjogren's syndrome.
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ERRγ agonist
GSK5182 is a highly selective inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM and does not interact with other nuclear receptors, including ERRα or ERα.
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- Sen He, .et al. The potential endocrine disruption mechanism of anthelmintic drug niclosamide by activating estrogen receptors and estrogen-related receptors, Toxicology, 2021, May 4;457:152805 PMID: 33961950
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hV1a receptor antagonist
Balovaptan (RG7314) is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors, and is used for the research of autism.
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Imidazoleacetic acid is an endogenous ligand that stimulates imidazole receptors.
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Dopamine receptor blocker
Dicarbine blocks dopamine receptors in various brain parts and prevents the depression of the conditioned defence reflexes caused by stimulation of the mesencephalic portion of the reticular formation. Dicarbine could be used to treat patients with schizophrenia and alcoholic psychosis in clinical.
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Adenosine A2A receptor antagonist
ST3932 is a metabolite of ST1535, acts as an antagonist of adenosine A2A receptor, with Kis of 8 nM and 33 nM for A2A and A1 receptors, respectively.
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partial agonist of GABA(A) receptor
RWJ-51204 is a partial agonist of GABA(A) receptor, with Ki of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.
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Bamirastine inhibits ligand binding to recombinant human histamine H1 receptors (rhH1R) with an IC50 value of 17.3 nM.
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5-HT2C receptor agonist
CP-809101 is a potent and selective 5-HT2C receptor agonist with pEC50 of 9.96/7.19/6.81 for human 5-HT2C/5-HT2B/5-HT2A receptors respectively.
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Orexin A human, rat, mouse is a 33 amino acid excitatory neuropeptide. Orexin A human, rat, mouse works on 2 specific G protein-coupled receptors (GPCRs): orexin-1 (OX1) and orexin-2 (OX2).
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PK14105 is a biological evaluation as a potential radioligand for PET studies of PBBS receptors.
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A3 adenosine receptor agonist
AB-MECA is a high affinity A3 adenosine receptor agonist, has high affinity for recombinant A1 and A3 receptors.
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κ-opioid receptor antagonist
JDTic is a highly selective antagonist for the κ-opioid receptor; without affecting the μ- or δ-opioid receptors.
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KOR antagonist
JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
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